126918-36-3

Upstream product

• 126918-21-6 (2R^*,3R^*)-2-(2,4-Difluorophenyl)-1,3-bis(methanesulfonyloxy)-2-butanol 
• 126918-20-5 (2R^*,3R^*)-2-(2,4-Difluorophenyl)-1,2,3-butanetriol 
• 150802-86-1 (1R)-1-<(2S)-2-(2,4-difluorophenyl)-2-oxiranyl>ethanol 
• 124-63-0 methanesulfonyl chloride 
• 126918-35-2 (1R)-1-<(2R)-2-(2,4-difluorophenyl)-2-oxiranyl>ethanol 
• 377078-82-5 [(1R)-1-[(2S)-2-(2,4-difluorophenyl)-2-oxiranyl]ethyl] benzoate 
• 138373-69-0 (1S)-1-<(2S)-2-(2,4-difluorophenyl)-2-oxiranyl>ethanol 
• 126918-18-1 (2S^*,3R^*)-2-(2,4-Difluorophenyl)-1-(dimethylisopropoxysilyl)-3-(tetrahydropyran-2-yloxy)-2-butanol 
• 126918-19-2 (2S,3S)-2-(2,4-Difluoro-phenyl)-3-(tetrahydro-pyran-2-yloxy)-butane-1,2-diol 
• 132563-81-6 1-(2,4-difluorophenyl)-2-(tetrahydropyranyloxy)propan-1-one 

Downstream Products

• 135270-10-9 (2S,3S)-2-(2,4-difluorophenyl)-3-methyl-2-(1H-1,2,4-triazol-1-yl)methyloxirane 
• 377078-85-8 (2S,3R)-3-(2,2-diethoxyethyl)amino-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-butanol 
• 377078-91-6 1-[(1R,2S)-2-(2,4-difluorophenyl)-2-hydroxy-1-methyl-3-(1H-1,2,4-triazol-1-yl)propyl]-3-[4-(1H-1-tetrazolyl)phenyl]-2-(1H,3H)-imidazolone 
• 377078-88-1 1-(2,2-diethoxyethyl)-1-[(1R,2S)-2-(2,4-difluorophenyl)-2-hydroxy-1-methyl-3-(1H-1,2,4-triazol-1-yl)propyl]-3-[4-(1H-1-tetrazolyl)phenyl]urea 
• 124627-86-7 1-(((2R,3S)-2-(2,4-difluorophenyl)-3-methyloxiran-2-yl)-methyl)-1H-1,2,4-triazole 

Relevant academic research and scientific papers

OPTICALLY ACTIVE HALOHYDRIN DERIVATIVE AND PROCESS FOR PRODUCING OPTICALLY ACTIVE EPOXY ALCOHOL DERIVATIVE FROM THE SAME

The present invention provides an industrially safe, easily operable process for producing an optically active epoxy alcohol derivative useful as an intermediate for pharmaceuticals from inexpensively available materials, and also provides a novel halohydrin derivative serving as an important intermediate for the epoxyalcohol derivative. Furthermore, the present invention provides a process for producing an intermediate for a triazole antifungal agent by allowing a halohydrin to react with a triazole sulfonamide, the process including a small number of steps. A process for producing an optically active epoxy alcohol derivative includes allowing an optically active α-substituted propionate derivative to react with a haloacetic acid derivative in the presence of a base to prepare an optically active haloketone derivative, allowing the resulting haloketone derivative to react with an aryl metal compound to stereoselectively prepare a halohydrin derivative, eliminating a substituent for the hydroxy group of the halohydrin derivative, and performing epoxidation with a base. Furthermore, a process for producing an intermediate for a triazole antifungal agent includes allowing a halohydrin derivative to react with a triazole sulfonamide, the process including a small number of steps.

PROCESS FOR PRODUCING EPOXYTRIAZOLE COMPOUND AND INTERMEDIATE THEREFOR

The present invention provides a compound of the formula (I); wherein Ar represents difluorophenyl group, which is useful as an intermediate in a process for producing an epoxytriazole compound of the formula (VII); wherein Ar represents difluorophenyl group, which is a synthetic intermediate of antifungal agents. The present invention also provides a process for producing a compound of the formula (VII) which comprises epoxydation step, deprotection step, reaction step with a compound represented by RSO2X, and reaction step with 1,2,4-triazole; or comprises epoxydation step, reaction step with 1,2,4-triazole, deprotection step, reaction step with a compound represented by RSO2X and treatment step by a base.

Optically active antifungal azoles. XIII. Synthesis of stereoisomers and metabolites of 1-[(1Rr,2R)-2-(2,4-difluorophenyl)-2-hydroxy-1-methyl-3(1H-1,2,4-triazol-1- yl)propyl]-3-[4-(1H-1-tetrazolyl)phenyl]-2-imidazolidinone (TAK-456)

1-[(1R,2R)-2-(2,4-Difluorophenyl)-2-hydroxy-1-methyl-3-(1H-1,2,4-triazol-1- yl)propyl]-3-[4-(1H-1-tetrazolyl)phenyll-2-imidazolidinone [(1R,2R)-1: TAK-456] is a new antifungal agent selected as a candidate for clinical trials. The three stereoisomers [(1S